1,3,4-Oxadiazoles: An emerging scaffold to target growth factors, enzymes and kinases as anticancer agents

Eur J Med Chem. 2015 Jun 5:97:124-41. doi: 10.1016/j.ejmech.2015.04.051. Epub 2015 Apr 27.

Abstract

Five member heterocyclic 1,3,4-oxadiazole nucleus find unique place in medicinal chemistry and plays significant role in producing anticancer activity. The small and simple 1,3,4-oxadiazole nucleus is present in various compounds involved in research aimed at evaluating new products that posses interesting pharmacological properties such as antitumour activity. Mono and 2,5-di-substituted-1,3,4-oxadiazole derivatives have attracted considerable attention owing to their effective biological activity and extensive use. The important mechanism involved during its tumour suppression is related with the inhibition of different growth factors, enzymes and kinases including telomerase enzyme, histone deacetylase (HDAC), methionine aminopeptidase (MetAP), thymidylate synthase (TS), glycogen synthase kinase-3 (GSK), epidermal growth factor (EGF), vascular endothelial growth factor (VEGF) and focal adhesion kinase (FAK). The focused criteria of this review is to highlights the targeted inhibitory activity of 1,3,4-oxadiazole derivatives and their structure activity relationship to generate potential anticancer agents.

Keywords: 1,3,4-Oxadiazole; Anticancer; Growth factors; Kinases; Telomerase enzyme.

Publication types

  • Review

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / therapeutic use*
  • Humans
  • Oxadiazoles / chemical synthesis
  • Oxadiazoles / chemistry
  • Oxadiazoles / therapeutic use*
  • Protein Kinases / drug effects*
  • Vascular Endothelial Growth Factors / drug effects*

Substances

  • Antineoplastic Agents
  • Oxadiazoles
  • Vascular Endothelial Growth Factors
  • 1,3,4-oxadiazole
  • Protein Kinases